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[酰基尿激酶及尿激酶组合在体外的纤溶和纤维蛋白原溶解作用]

[Fibrinolytic and fibrinogenolytic effects of acyl urokinase and urokinase combinations in vitro].

作者信息

Mukhametova L I, Aĭsina R B, Varfolomeev S D

出版信息

Bioorg Khim. 2006 Jul-Aug;32(4):384-90. doi: 10.1134/s1068162006040042.

DOI:10.1134/s1068162006040042
PMID:16909862
Abstract

The in vitro thrombolytic and side effects of double-strand urokinase-type plasminogen activator (tcu-PA), p-guanidinobenzoyl tcu-PA (GB-tcu-PA), and their combinations were compared. The reversible blocking of the active site stabilizes GB-tcu-PA in human plasma and results in longer thrombolysis and lesser side effects than those of tcu-PA. However, the acylated activator displays a marked lag period of thrombolytic action. GB-tcu-PA and tcu-PA combinations (molar ratios 4 : 1 and 1 : 1) induce a prolonged and effective thrombolysis without the initial lag period at a low level of plasminogen, fibrinogen, and alpha2-antiplasmin depletion in the plasma surrounding the clot.

摘要

比较了双链尿激酶型纤溶酶原激活剂（tcu-PA）、对胍基苯甲酰tcu-PA（GB-tcu-PA）及其组合的体外溶栓作用和副作用。活性位点的可逆性阻断使GB-tcu-PA在人血浆中更稳定，与tcu-PA相比，其溶栓时间更长，副作用更小。然而，酰化激活剂表现出明显的溶栓作用延迟期。GB-tcu-PA与tcu-PA的组合（摩尔比4:1和1:1）在纤溶酶原、纤维蛋白原和α2-抗纤溶酶水平较低的情况下，能在不出现初始延迟期的情况下诱导延长且有效的溶栓作用，同时在血凝块周围血浆中的消耗较少。

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Bioorg Khim. 2006 Jul-Aug;32(4):384-90. doi: 10.1134/s1068162006040042.
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